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Preparation with solid lipid nano-particle as podophyllotoxin and its derivative carrier

A solid lipid nano-podophyllotoxin technology, which is applied in liposome delivery, drug combination, anti-tumor drugs, etc., can solve the problems of easy formation of drug resistance, poor water solubility, narrow anti-tumor spectrum, etc., to improve biological High utilization rate, encapsulation rate, and film-forming effect

Inactive Publication Date: 2007-06-20
TONGJI UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

However, they still have the following disadvantages: poor water solubility, narrow anti-tumor spectrum, easy inactivation through metabolism, easy to form drug resistance and severe bone marrow suppression and other toxic effects, which limit their wide application in clinical practice.

Method used

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  • Preparation with solid lipid nano-particle as podophyllotoxin and its derivative carrier
  • Preparation with solid lipid nano-particle as podophyllotoxin and its derivative carrier
  • Preparation with solid lipid nano-particle as podophyllotoxin and its derivative carrier

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0040] Take 100mg of stearic acid and 5ml of acetone and put them into a 25ml stoppered pear-shaped bottle, ultrasonically dissolve them fully, add 100mg of lecithin in chloroform, heat to dissolve, and form an organic phase. Another 300mg of Myrj59 was dissolved in 30ml of high-purity water to form the aqueous phase. Dilute the organic phase with 6 # Inject the water phase at (75±2)°C stirred at 1000r / min with the needle, and continue to stir for about 4 hours to completely evaporate the organic solvent and concentrate the system to about 5ml, and quickly mix the obtained translucent system in another 0-2°C 10ml of the aqueous phase stirred at 1000r / min was stirred for 2 hours to obtain a blank solid lipid nanoparticle suspension, and the system was adjusted to 20ml. The obtained blank solid lipid nanoparticle suspension is a stable colloidal dispersion system with uniform appearance, uniform size and uniform distribution, and an average particle diameter of 50.4nm through t...

Embodiment 2

[0042] Take 10mg of podophyllotoxin, 100mg of stearic acid, and 5ml of acetone, put them into a 25ml stoppered pear-shaped bottle, dissolve them fully by ultrasonication, add 100mg of lecithin in chloroform, heat to dissolve, and form an organic phase. Another 200mg of Myrj59 was dissolved in 30ml of high-purity water to form the water phase. Dilute the organic phase with 6 # Inject the water phase at (75±2)°C stirred at 1000r / min with the needle, and continue to stir for about 4 hours to completely evaporate the organic solvent and concentrate the system to about 5ml, and quickly mix the obtained translucent system in another 0-2°C 10ml of the aqueous phase stirred at 1000r / min, and continued to stir for 2h to obtain the podophyllin solid lipid nanoparticle suspension, and the volume of the system was adjusted to 20ml. Take the podophyllin solid lipid nanoparticle suspension and dilute it with high-purity water, and measure the particle size distribution of the nanoparticle ...

Embodiment 3

[0044] Obtain podophyllotoxin derivative solid lipid nanoparticle suspension with the method in embodiment 2, can find out that gained podophyllotoxin derivative solid lipid nanoparticle size is uniform, uniformly distributed, and average particle size is 54.4nm, see Figure 3.

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Abstract

An application of the solid liposome nanoparticles as the carrier of podophyllotoxin and its derivative and a composite medicine containing podophyllotoxin or its derivative and said solid liposome nanoparticles as carrier are disclosed. Its advantages are higher curative effect, high stability and low cost.

Description

technical field [0001] The invention relates to the application of solid lipid nanoparticle as a carrier of podophyllotoxin and its derivatives and its new dosage form. Background technique [0002] Solid lipid nanoparticles (SLN) is a new type of lipid drug-loading system that has been developing in the past ten years. It is based on natural or synthetic high melting point solid lipids (such as saturated fatty acid glycerides). , stearic acid, mixed lipid) as the carrier, the nano drug delivery system made by adsorbing or encapsulating the drug in the lipid core. Similar to emulsions and liposomes, SLN uses lipid materials with low toxicity and good biocompatibility as carriers. At the same time, the solid lipid makes it have the advantages of polymer nanoparticles (PNP), such as controlled release of drugs, avoiding degradation or leakage of drugs, and good targeting. SLN's water dispersion system can be sterilized by autoclaving or γ-irradiation, and has long-term physi...

Claims

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Application Information

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IPC IPC(8): A61K31/365A61K9/127A61P35/00
Inventor 汪世龙孙晓宇张蕤聂庆姚思德
Owner TONGJI UNIV
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